Urea, N-[2-[4-hydroxy-4-(phenylmethyl)-1-piperidinyl]ethyl]-N'-(2-Methyl-4-quinolinyl)-
更新时间：2021-07-26 18:31:37
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| 常用名 | ACT 058362; PALOSURAN, | CAS号 | 540769-28-6 |
|---|---|---|---|
| 价格 | $需询单/100g $需询单/1kg $需询单/100kg $需询单/1000kg | 纯度 | 98.0% |
| 备货期 | 需询单 | 库存 | 询单 |
| 产品详情（用途，包装等）
用途： Palosuran (ACT-058362) is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6±0.2 nM. IC50 Value: 3.6±0.2 nM [1]Target: Urotensin Receptor (GPR14)in vitro: Palosuran inhibited 125I-U-II binding to human UT receptors in membrane preparations from CHO cells carrying the human UT receptors almost as potently as cold U-II, with an IC50 of 3.6 ± 0.2 nM. On cells, the inhibitory binding potency of palosuran against human UT receptor was lower than on membranes (IC50 = 46.2 ± 13 nM on TE 671 cells and 86 ± 30 nM on recombinant CHO cells). Compared with the human UT receptor, the binding inhibitory potency of palosuran against the rat UT receptor was lower in membrane preparation (400-fold), as well as in cells (>120-fold) [1].in vivo: Long-term treatment of streptozotocin-induced diabetic rats with palosuran improved survival, increased insulin, and slowed the increase in glycemia, glycosylated hemoglobin, and serum lipids. Furthermore, palosuran increased renal blood flow and delayed the development of proteinuria and renal damage [2]. Palosuran was rapidly absorbed with maximum plasma concentrations at 1 hour after drug administration. The accumulation factor was 1.7 (geometric mean) (95% confidence interval, 1.3 to 2.1).Palosuran was well tolerated [3]. In mesenteric vessels, palosuran treatment up-regulated expression of RhoA and Rho-kinase, increased Rho-kinase-activity, and diminished nitric oxide (NO)/cyclic guanosine 3',5'-monophosphate (cGMP) signaling. Moreover, palosuran increased renal blood flow, sodium, and water excretion in BDL rats [4].Toxicity: Palosuran was well tolerated. No serious adverse events or dose-related adverse events were reported. No treatment-related pattern was detected for vital signs, clinical laboratory parameters, or electrocardiography parameters [5]. 物理化学性质： CAS号：540769-28-6 常用中文名：ACT 058362; PALOSURAN, 常用英文名：Palosuran 分子式：C25H30N4O2 分子量：418.53100 密度：N/A 沸点：N/A 熔点：N/A 闪点：N/A 储存条件：-20℃ |
达阳化工（杭州）有限公司
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地区： 浙江省 杭州市 西湖区
联系人：王小姐
联系人电话：+86-571-8893-8639
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主要市场：Mainly in Southeast Asia and European and American markets
年贸易额：10 to 20 million USD
外贸占销售比例：90%
主要合作伙伴：
- 上海化源世纪贸易有限公司
- 上海市 上海市 普陀区
- 产品名：Palosuran
- 价格：
- 纯度：98.0%
- 备货期：10天
- 联系人：徐经理
- 上海阿拉丁生化科技股份有限公司
- 上海市 上海市 浦东新区
- 产品名：Palosuran
- 价格： ￥539.9/25mg ￥269.9/10mg ￥850.9/50mg ￥1445.9/100mg
- 纯度：98.0%
- 备货期：1天
- 联系人：阿拉丁
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参考价格：$290/10mM*1mLinDMSO